Chemistry:ARM390
From HandWiki
Short description: Opioid-analgesic compound
 | This article relies largely or entirely on a single source. (November 2024) |
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| Other names | ARM-390 |
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| Formula | C23H28N2O |
| Molar mass | 348.490 g·mol−1 |
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ARM-390 is an opioid-analgesic compound selective for the delta opioid receptor.[1][2][3]
It is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.[1]
In contrast to the delta-opioid selective agonist SNC-80, ARM390 was not found to produce receptor desensitization following multiple administrations. Although behavioral desensitization formed to the analgesic effect of ARM390 through a receptor internalization-independent mechanism, anxiolytic effects persisted during long-term treatment.[4] ARM390 has been dubbed a "low-internalizing agonist" of delta opioid receptors.[4]
References
- ↑ 1.0 1.1 "N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues". Journal of Medicinal Chemistry 43 (21): 3895–3905. October 2000. doi:10.1021/jm000229p. PMID 11052794.
- ↑ "Pharmacological characterization of AR-M1000390 at human delta opioid receptors". Life Sciences 73 (13): 1691–1704. August 2003. doi:10.1016/s0024-3205(03)00489-2. PMID 12875901.
- ↑ "Ligand-directed trafficking of the δ-opioid receptor in vivo: two paths toward analgesic tolerance". The Journal of Neuroscience 30 (49): 16459–16468. December 2010. doi:10.1523/JNEUROSCI.3748-10.2010. PMID 21147985.
- ↑ 4.0 4.1 "The delta opioid receptor: an evolving target for the treatment of brain disorders". Trends in Pharmacological Sciences 32 (10): 581–590. October 2011. doi:10.1016/j.tips.2011.06.008. PMID 21925742.
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